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Assay Detail

CHEMBL5366077

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant PRMT9 using biotinylated SF3B2(500 to 519 residues) as substrate and SAM as cosubstrate pre-incubated with compound for 30 mins followed by substrate addition measured after 60 mins by AlphaLISA assay
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 9 (CHEMBL4105724)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor.
Feoli A, Iannelli G, Cipriano A, Milite C, Shen L, Wang Z, Hadjikyriacou A, Lowe TL, Safaeipour C, Viviano M, Sarno G, Morretta E, Monti MC, Yang Y, Clarke SG, Cosconati S, Castellano S, Sbardella G.
J Med Chem (2023) 66 : 13665 -13683
PubMed 37560786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.81 6.70
Inhibition 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5396270 1 6.70
CHEMBL5199380 1 6.05
CHEMBL5406557 1 5.99
CHEMBL5202088 1 5.92
CHEMBL5186617 1 5.89
CHEMBL5170047 1 5.88
CHEMBL5408585 1 5.61
CHEMBL5206272 1 5.24
CHEMBL5173678 1 5.03
CHEMBL5191769 1 -
CHEMBL2179359 1 -
CHEMBL5426910 1 -
CHEMBL2179350 1 -
CHEMBL5394196 1 -
CHEMBL5430799 1 -
CHEMBL5420873 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5396270 IC50 = 200.0 nM 6.70
CHEMBL5199380 IC50 = 890.0 nM 6.05
CHEMBL5406557 IC50 = 1020.0 nM 5.99
CHEMBL5202088 IC50 = 1200.0 nM 5.92
CHEMBL5186617 IC50 = 1300.0 nM 5.89
CHEMBL5170047 IC50 = 1320.0 nM 5.88
CHEMBL5408585 IC50 = 2470.0 nM 5.61
CHEMBL5206272 IC50 = 5800.0 nM 5.24
CHEMBL5173678 IC50 = 9300.0 nM 5.03
CHEMBL5191769 IC50 > 10000.0 nM -
CHEMBL2179359 Inhibition - % -
CHEMBL5426910 Inhibition - % -
CHEMBL2179350 Inhibition - % -
CHEMBL5394196 Inhibition - % -
CHEMBL5430799 Inhibition - % -
CHEMBL5420873 Inhibition - % -